Category: 1351413-50-7

Zhang, Yongda published the artcileAn Enantioselective Synthesis of an 11-β-HSD-1 Inhibitor via an Asymmetric Methallylation Catalyzed by (S)-3,3′-F₂-BINOL, Name: (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, the publication is Journal of Organic Chemistry (2016), 81(6), 2665-2669, database is CAplus and MEDLINE.

An efficient asym. synthesis of 11-β-HSD inhibitor I has been accomplished in five linear steps and 53% overall yield, starting from the readily available 3-chloro-1-phenylpropan-1-one. The key feature of the synthesis includes an asym. methallylation of 3-chloro-1-phenylpropan-1-one catalyzed by the highly effective organocatalyst (S)-3,3′-F₂-BINOL under solvent-free and metal-free conditions.

Journal of Organic Chemistry published new progress about 1351413-50-7. 1351413-50-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Pyridine,Boronic Acids,Boronic acid and ester, name is (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, and the molecular formula is C11H8ClN3, Name: (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Patel, Nitinchandra D. published the artcileEffective BI-DIME Ligand for Suzuki-Miyaura Cross-Coupling Reactions in Water with 500 ppm Palladium Loading and Triton X, Product Details of C6H8BNO3, the publication is Asian Journal of Organic Chemistry (2017), 6(9), 1285-1291, database is CAplus.

An efficient, sustainable, and broadly applicable procedure has been developed for Suzuki-Miyaura cross-coupling reactions in environmentally benign solvent (water) by employing as little as 500 ppm Pd(OAc)₂ with a monophosphorus BI-DIME ligand in the presence of inexpensive and com. available nonionic surfactant Triton X-100. This method was applied to a broad range of functionalized reaction partners, thereby affording excellent yields of the coupling products, including active pharmaceutical ingredients (APIs). An interesting kinetic study by using reaction calorimetry is also presented, which describes the effect of reaction parameters that enabled the low catalyst loading.

Asian Journal of Organic Chemistry published new progress about 1351413-50-7. 1351413-50-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Pyridine,Boronic Acids,Boronic acid and ester, name is (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, and the molecular formula is C6H8BNO3, Product Details of C6H8BNO3.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Kale, Manoj G. published the artcileThiazolopyridine Ureas as Novel Antitubercular Agents Acting through Inhibition of DNA Gyrase B, Category: pyridine-derivatives, the publication is Journal of Medicinal Chemistry (2013), 56(21), 8834-8848, database is CAplus and MEDLINE.

A pharmacophore-based search led to the identification of thiazolopyridine ureas, e.g., I, as a novel scaffold with antitubercular activity acting through inhibition of DNA Gyrase B (GyrB) ATPase. Evaluation of the binding mode of thiazolopyridines in a Mycobacterium tuberculosis (Mtb) GyrB homol. model prompted exploration of the side chains at the thiazolopyridine ring C-5 position to access the ribose/solvent pocket. Potent compounds with GyrB IC₅₀ â‰?1 nM and Mtb MIC â‰?0.1 μM were obtained with certain combinations of side chains at the C-5 position and heterocycles at the C-6 position of the thiazolopyridine core. Substitutions at C-5 also enabled optimization of the physicochem. properties. Representative compounds were cocrystd. with Streptococcus pneumoniae (Spn) ParE; these confirmed the binding modes predicted by the homol. model. The target link to GyrB was confirmed by genetic mapping of the mutations conferring resistance to thiazolopyridine ureas. The compounds are bactericidal in vitro and efficacious in vivo in an acute murine model of tuberculosis.

Journal of Medicinal Chemistry published new progress about 1351413-50-7. 1351413-50-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Pyridine,Boronic Acids,Boronic acid and ester, name is (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, and the molecular formula is C6H8BNO3, Category: pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Latli, Bachir published the artcilePotent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 labeled with carbon-13 and carbon-14, Recommanded Product: (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, the publication is Journal of Labelled Compounds and Radiopharmaceuticals (2017), 60(9), 420-430, database is CAplus and MEDLINE.

(S)-6-(2-Hydroxy-2-methylpropyl)-3-((S)-1-(4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl)ethyl)-6-phenyl-1,3-oxazinan-2-one (I) and (4aR,9aS)-1-(1H-benzo[d]midazole-5-carbonyl)-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-b]pyridine-6-carbonitrile hydrochloride (II) are potent and selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 enzyme. These 2 drug candidates developed for the treatment of type-2 diabetes were prepared labeled with carbon-13 and carbon-14 to enable drug metabolism, pharmacokinetics, bioanal., and other studies. In the carbon-13 synthesis, benzoic-¹³C₆ acid was converted in 7 steps and in 16% overall yield to [¹³C₆]-I. Aniline-¹³C₆ was converted in 7 steps to 1H-benzimidazole-1-2,3,4,5,6-¹³C₆-5-carboxylic acid and then coupled to a tricyclic chiral indenopiperidine to afford [¹³C₆]-II in 19% overall yield. The carbon-14 labeled I was prepared efficiently in 2 radioactive steps in 41% overall yield from an advanced intermediate using carbon-14 labeled Me magnesium iodide and Suzuki-Miyaura cross coupling via in situ boronate formation. As for the synthesis of [¹⁴C]-II, 1H-benzimidazole-5-carboxylic-¹⁴C acid was first prepared in 4 steps using potassium cyanide-¹⁴C, then coupled to the chiral indenopiperidine using amide bond formation conditions in 26% overall yield.

Journal of Labelled Compounds and Radiopharmaceuticals published new progress about 1351413-50-7. 1351413-50-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Pyridine,Boronic Acids,Boronic acid and ester, name is (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid, and the molecular formula is C6H8BNO3, Recommanded Product: (1-Methyl-2-oxo-1,2-dihydropyridin-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem